Angina:
Indications for: TOPROL-XL
Angina pectoris.
Clinical Trials:
Angina Pectoris
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Controlled clinical studies have shown that the immediate-release formulation of metoprolol at dosages of 100 to 400 mg once daily was effective as an antianginal agent, reducing the number of angina attacks and increasing exercise tolerance.
Adult Dosage:
Initially 100mg once daily. May increase at 1-week intervals; max 400mg/day.
Children Dosage:
Not established.
TOPROL-XL Contraindications:
Severe bradycardia. 2nd- or 3rd-degree heart block. Cardiogenic shock. Decompensated heart failure. Sick sinus syndrome (unless paced).
TOPROL-XL Warnings/Precautions:
Mild or compensated heart failure. Ischemic heart or peripheral vascular disease. 1st-degree AV block. Sinus node dysfunction. Conduction disorders (eg, Wolff-Parkinson-White). Monitor HR during therapy. Bronchospastic disease. Pheochromocytoma. Surgery. Diabetes. May mask signs and increase risk for hypoglycemia. Hyperthyroidism. Avoid abrupt cessation. Hepatic impairment. Elderly. Neonates. Pregnancy. Nursing mothers: monitor infants.
TOPROL-XL Classification:
Beta-blocker.
TOPROL-XL Interactions:
May potentiate hypotension or marked bradycardia with catecholamine depleting drugs (eg, reserpine, MAOIs). Potentiated by strong CYP2D6 inhibitors (eg, quinidine, fluoxetine, paroxetine, propafenone); monitor if unavoidable. Increased risk of bradycardia with glycosides, clonidine, diltiazem, verapamil. May block epinephrine.
Adverse Reactions:
Fatigue, dizziness, depression, diarrhea, dyspnea, bradycardia, rash; heart block, MI, angina.
Drug Elimination:
- Renal. Half-life: 3–7hrs.
Generic Drug Availability:
YES
How Supplied:
Tabs—100, 1000
CHF and arrhythmias:
Indications for: TOPROL-XL
Heart failure, to reduce the risk of cardiovascular mortality and heart failure hospitalizations in patients with heart failure.
Clinical Trials:
Heart Failure
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The randomized, double-blind, placebo-controlled MERIT-HF study evaluated the efficacy of Toprol-XL in 3991 patients with ejection fraction ≤0.40 and NYHA Class II-IV heart failure attributable to ischemia, hypertension, or cardiomyopathy. Patients were randomly assigned 1:1 to receive Toprol-XL or placebo. The primary endpoints of the trial were (1) all-cause mortality plus all-cause hospitalization (time to first event) and (2) all-cause mortality.
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The trial was terminated early for a statistically significant reduction in all-cause mortality (34%, nominal P =.00009).
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The risk of all-cause mortality plus all-cause hospitalization was reduced by 19% (P =.00012). The trial also showed improvements in heart failure-related mortality and heart failure-related hospitalizations, and NYHA functional class.
Adult Dosage:
Class II: initially 25mg once daily; more severe: 12.5mg once daily. May double dose as tolerated every 2 weeks; reduce if symptomatic bradycardia occurs; max 200mg/day.
Children Dosage:
Not established.
TOPROL-XL Contraindications:
Severe bradycardia. 2nd- or 3rd-degree heart block. Cardiogenic shock. Decompensated heart failure. Sick sinus syndrome (unless paced).
TOPROL-XL Warnings/Precautions:
Mild or compensated heart failure. Ischemic heart or peripheral vascular disease. 1st-degree AV block. Sinus node dysfunction. Conduction disorders (eg, Wolff-Parkinson-White). Monitor HR during therapy. Bronchospastic disease. Pheochromocytoma. Surgery. Diabetes. May mask signs and increase risk for hypoglycemia. Hyperthyroidism. Avoid abrupt cessation. Hepatic impairment. Elderly. Neonates. Pregnancy. Nursing mothers: monitor infants.
TOPROL-XL Classification:
Beta-blocker.
TOPROL-XL Interactions:
May potentiate hypotension or marked bradycardia with catecholamine depleting drugs (eg, reserpine, MAOIs). Potentiated by strong CYP2D6 inhibitors (eg, quinidine, fluoxetine, paroxetine, propafenone); monitor if unavoidable. Increased risk of bradycardia with glycosides, clonidine, diltiazem, verapamil. May block epinephrine.
Adverse Reactions:
Fatigue, dizziness, depression, diarrhea, dyspnea, bradycardia, rash; heart block, MI, angina.
Drug Elimination:
- Renal. Half-life: 3–7hrs.
Generic Drug Availability:
YES
How Supplied:
Tabs—100, 1000
Hypertension:
Indications for: TOPROL-XL
Hypertension.
Clinical Trials:
Hypertension
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A double-blind study evaluated the efficacy of Toprol-XL in 1092 patients with mild to moderate hypertension. Patients were randomly assigned to receive once daily Toprol-XL (25, 100, or 400 mg), Plendil (felodipine extended-release tablets), the combination, or placebo. Results showed that treatment with Toprol-XL alone decreased sitting BP by 6–8/4–7 mmHg (placebo-corrected change from baseline) at 24 hours post-dose after 9 weeks. The combination of Toprol-XL and Plendil had greater effects on BP.
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In controlled clinical studies, an immediate-release dosage form of metoprolol (100–450 mg daily) achieved effective antihypertensive effects when used alone or as concomitantly with thiazide-type diuretics. Toprol-XL at dosages of 100–400 mg once daily had similar results as conventional metoprolol tablets administered 2 to 4 times daily. Moreover, Toprol-XL 50 mg once daily lowered blood pressure 24 hours post-dosing in placebo-controlled studies.
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In controlled, comparative clinical studies, immediate-release dosage form of metoprolol was observed to be comparable to propranolol, methyldopa, and thiazide-type diuretics, and affected both supine and standing BP.
Adult Dosage:
Initially 25–100mg once daily, alone or with a diuretic. May increase at 1-week intervals; max 400mg/day.
Children Dosage:
<6yrs: not established. ≥6yrs: initially 1mg/kg once daily; max 50mg/day. Adjust based on response. Max 2mg/kg (200mg) daily.
TOPROL-XL Contraindications:
Severe bradycardia. 2nd- or 3rd-degree heart block. Cardiogenic shock. Decompensated heart failure. Sick sinus syndrome (unless paced).
TOPROL-XL Warnings/Precautions:
Mild or compensated heart failure. Ischemic heart or peripheral vascular disease. 1st-degree AV block. Sinus node dysfunction. Conduction disorders (eg, Wolff-Parkinson-White). Monitor HR during therapy. Bronchospastic disease. Pheochromocytoma. Surgery. Diabetes. May mask signs and increase risk for hypoglycemia. Hyperthyroidism. Avoid abrupt cessation. Hepatic impairment. Elderly. Neonates. Pregnancy. Nursing mothers: monitor infants.
TOPROL-XL Classification:
Cardioselective beta-blocker.
TOPROL-XL Interactions:
May potentiate hypotension or marked bradycardia with catecholamine depleting drugs (eg, reserpine, MAOIs). Potentiated by strong CYP2D6 inhibitors (eg, quinidine, fluoxetine, paroxetine, propafenone); monitor if unavoidable. Increased risk of bradycardia with glycosides, clonidine, diltiazem, verapamil. May block epinephrine.
Adverse Reactions:
Fatigue, dizziness, depression, diarrhea, dyspnea, bradycardia, rash; heart block, MI, angina.
Drug Elimination:
- Renal. Half-life: 3–7hrs.
Generic Drug Availability:
YES
How Supplied:
Tabs—100, 1000
